Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables

The aim of this study is to evaluate the cooperative interactions between formulation variables of ropinirole transdermal patches and characterize the effects of drug loading and crystallinity, degree of ionization and drug-polymer solubilization, functionalization of acrylate polymeric basis, and t...

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Autores: Paterna-Paterna, Jesús, Miñarro Carmona, Montserrat, Pujol Dilmé, M. Dolors, Ticó Grau, Josep R., Boix Montañés, Antonio de Pádua
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/184976
Acceso en línea:https://hdl.handle.net/2445/184976
Access Level:acceso abierto
Palabra clave:Polímers
Sistemes d'alliberament de medicaments
Medicació transdèrmica
Polymers
Drug delivery systems
Transdermal medication
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spelling Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation VariablesPaterna-Paterna, JesúsMiñarro Carmona, MontserratPujol Dilmé, M. DolorsTicó Grau, Josep R.Boix Montañés, Antonio de PáduaPolímersSistemes d'alliberament de medicamentsMedicació transdèrmicaPolymersDrug delivery systemsTransdermal medicationThe aim of this study is to evaluate the cooperative interactions between formulation variables of ropinirole transdermal patches and characterize the effects of drug loading and crystallinity, degree of ionization and drug-polymer solubilization, functionalization of acrylate polymeric basis, and the addition of permeation enhancers over the release profiles. Several series of transdermal films based on carboxylic or hydroxylic acrylates (DuroTak®) and containing 1 to 10% ropinirole hydrochloride were laminated by mold-casting and evaporation. Formulations were characterized for crystallinity, drug particle size, drug assay, and residual solvents. Release profiles were obtained at different drug ionization state using paddle over disk apparatus. Mechanisms were elucidated with nonlinear data fitting of relevant release equations. Fickian and erosion processes were evaluated with the Peppas-Sahlin equation, and burst release risks were estimated as an independent term added to Higuchi kinetics. X-ray diffraction and microscopy evidenced differences in drug-polymer solubilization and density of drug crystals. Concerning drug release, area under the curve of dissolved quantities and release percentage were discriminant variables in mutual influence. Peppas-Shalin equation was the majority descriptor of release suggesting a combination of Fickian and erosion processes, revealing a decrease in the Fickian component as drug loading increased. Major burst release risks were evidenced mostly with Higuchi kinetics with vinylacetate acrylates. The carboxylic polymer without vinylacetate provided the best release extent, being more highly efficient as lower the drug loading was. Permeation enhancers with carboxylic or aliphatic radicals have, additionally, modified the release properties of ropinirole. Chemical interactions between the drug and acrylic polymers have been demonstrated. Only the effect with carboxylic polymer is pH dependent. The vinyl acetate comonomer reduces the drug release rate most effectively in formulations with low drug loads. The acrylic polymers without vinylacetate achieved the highest drug solubilization and thus the highest degree of release, providing a release of approximately 15% of the drug load. Keywords: Acrylate-vinylacetate copolymer; Drug loading; Release; Ropinirole; Transdermal.American Association of Pharmaceutical Scientists2022info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://hdl.handle.net/2445/184976Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésReproducció del document publicat a: https://doi.org/10.1208/s12249-022-02238-4AAPS PharmSciTech, 2022, vol. 23, num. 82, p. 1-14https://doi.org/10.1208/s12249-022-02238-4cc by (c) Jesús Paterna-Paterna, et al., 2022http://creativecommons.org/licenses/by/3.0/es/info:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1849762026-05-27T06:46:51Z
dc.title.none.fl_str_mv Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
title Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
spellingShingle Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
Paterna-Paterna, Jesús
Polímers
Sistemes d'alliberament de medicaments
Medicació transdèrmica
Polymers
Drug delivery systems
Transdermal medication
title_short Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
title_full Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
title_fullStr Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
title_full_unstemmed Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
title_sort Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables
dc.creator.none.fl_str_mv Paterna-Paterna, Jesús
Miñarro Carmona, Montserrat
Pujol Dilmé, M. Dolors
Ticó Grau, Josep R.
Boix Montañés, Antonio de Pádua
author Paterna-Paterna, Jesús
author_facet Paterna-Paterna, Jesús
Miñarro Carmona, Montserrat
Pujol Dilmé, M. Dolors
Ticó Grau, Josep R.
Boix Montañés, Antonio de Pádua
author_role author
author2 Miñarro Carmona, Montserrat
Pujol Dilmé, M. Dolors
Ticó Grau, Josep R.
Boix Montañés, Antonio de Pádua
author2_role author
author
author
author
dc.subject.none.fl_str_mv Polímers
Sistemes d'alliberament de medicaments
Medicació transdèrmica
Polymers
Drug delivery systems
Transdermal medication
topic Polímers
Sistemes d'alliberament de medicaments
Medicació transdèrmica
Polymers
Drug delivery systems
Transdermal medication
description The aim of this study is to evaluate the cooperative interactions between formulation variables of ropinirole transdermal patches and characterize the effects of drug loading and crystallinity, degree of ionization and drug-polymer solubilization, functionalization of acrylate polymeric basis, and the addition of permeation enhancers over the release profiles. Several series of transdermal films based on carboxylic or hydroxylic acrylates (DuroTak®) and containing 1 to 10% ropinirole hydrochloride were laminated by mold-casting and evaporation. Formulations were characterized for crystallinity, drug particle size, drug assay, and residual solvents. Release profiles were obtained at different drug ionization state using paddle over disk apparatus. Mechanisms were elucidated with nonlinear data fitting of relevant release equations. Fickian and erosion processes were evaluated with the Peppas-Sahlin equation, and burst release risks were estimated as an independent term added to Higuchi kinetics. X-ray diffraction and microscopy evidenced differences in drug-polymer solubilization and density of drug crystals. Concerning drug release, area under the curve of dissolved quantities and release percentage were discriminant variables in mutual influence. Peppas-Shalin equation was the majority descriptor of release suggesting a combination of Fickian and erosion processes, revealing a decrease in the Fickian component as drug loading increased. Major burst release risks were evidenced mostly with Higuchi kinetics with vinylacetate acrylates. The carboxylic polymer without vinylacetate provided the best release extent, being more highly efficient as lower the drug loading was. Permeation enhancers with carboxylic or aliphatic radicals have, additionally, modified the release properties of ropinirole. Chemical interactions between the drug and acrylic polymers have been demonstrated. Only the effect with carboxylic polymer is pH dependent. The vinyl acetate comonomer reduces the drug release rate most effectively in formulations with low drug loads. The acrylic polymers without vinylacetate achieved the highest drug solubilization and thus the highest degree of release, providing a release of approximately 15% of the drug load. Keywords: Acrylate-vinylacetate copolymer; Drug loading; Release; Ropinirole; Transdermal.
publishDate 2022
dc.date.none.fl_str_mv 2022
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/184976
url https://hdl.handle.net/2445/184976
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Reproducció del document publicat a: https://doi.org/10.1208/s12249-022-02238-4
AAPS PharmSciTech, 2022, vol. 23, num. 82, p. 1-14
https://doi.org/10.1208/s12249-022-02238-4
dc.rights.none.fl_str_mv cc by (c) Jesús Paterna-Paterna, et al., 2022
http://creativecommons.org/licenses/by/3.0/es/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv cc by (c) Jesús Paterna-Paterna, et al., 2022
http://creativecommons.org/licenses/by/3.0/es/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv American Association of Pharmaceutical Scientists
publisher.none.fl_str_mv American Association of Pharmaceutical Scientists
dc.source.none.fl_str_mv Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15.301603

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